title: 5-Nitroisatin-derived thiosemicarbazones: potential antileishmanial agents.
abstract: A series of 29 previously reported N(4)-substituted 5-nitroisatin-3-thiosemicarbazones 2-30 has been screened for leishmanicidal potential. Compounds 2-4, 7, 8, 10-13, 15-19, 21, 23, 24, 26, 28 and 30 exhibited good to excellent antileishmanial activities with IC50 values ranging from 0.44 ± 0.02 to 32.38 ± 0.66 µg/mL. Of these, 5, 7, 19 and 28 proved to be the most active antileishmanial agents, displaying activities with IC50 values 1.78 ± 0.35, 0.44 ± 0.02, 1.91 ± 0.04 and 4.28 ± 0.75 µg/mL, respectively, which were even better than the standard drug, pentamidine (IC50 = 5.09 ± 0.04 µg/mL). This study presents the first example of exhibition of leishmanicidal potential by isatin-thiosemicarbazones and as such furnishes a solid basis for further research on these compounds to develop more potent antileishmanial agents.
authors.affiliation: Institute of Chemical Sciences, Organic Chemistry Division, Bahauddin Zakariya University , Multan , Pakistan and.
authors.forename: Humayun
authors.initials: H
authors.lastname: Pervez
authors.forename: Nazia
authors.initials: N
authors.lastname: Manzoor
authors.forename: Muhammad
authors.initials: M
authors.lastname: Yaqub
authors.forename: Khalid Mohammed
authors.initials: KM
authors.lastname: Khan
mesh_terms: D004305:Dose-Response Relationship, Drug; D007510:Isatin / Q000031:analogs & derivatives / Q000737:chemistry*; D018320:Leishmania major / Q000187:drug effects*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D013882:Thiosemicarbazones; D014344:Trypanocidal Agents; D007510:Isatin
keywords: Isatin-thiosemicarbazones; Leishmania major; leishmanicidal activity